Microencapsulation of ketorolac tromethamine by means of a coacervation-phase separation technique induced by the addition of non-solvent.
Ketorolac tromethamine (KT) is a non-steroidal drug with potent analgesic and anti-inflammatory activity and is absorbed rapidly (Tmax < 1.0 h) with an efficiency > 87% following oral and intramuscular administration. The plasma half-life of ketorolac ranges from 1.1 to 6.0 h. Its oral bioavailability is estimated to be 80%. Ketorolac has been found 36 times more potent than phenylbutazone, approximately twice as potent as indomethacin, and three times more potent than naproxen in suppressing carrageenan-induced paw oedema in rat. In this study, microcapsules of KT were prepared by means of coacervation-phase separation technique induced by the addition of non-solvent, and release rates from microcapsules were studied. Eudragit S100 was used as the coating material. Coacervation was achieved by the addition of cyclohexane at 2 ml/min at 25 degrees C and 1:4 solvent: non-solvent ratio was used. The microcapsules were washed with cyclohexane to harden the wall and dried at room temperature. Microcapsules with core:wall ratio of 1:1 and 1:2 were prepared and the particles obtained by sieving with an average diameter of 177-500 microns were used. The yield was calculated and the release properties of KT were investigated by USP XXII paddle method and using UV spectrophotometry at 318 and 323 nm.
Genç
L
L
Faculty of Pharmacy, Department of Pharmaceutical Technology, Anadolu University, Eskisehir, Turkey.
Demirel
M
M
Güler
E
E
Hegazy
N
N
D000180:Acrylic Resins / Q000737:chemistry; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry*; D002214:Capsules; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D020911:Ketorolac Tromethamine; D011109:Polymethacrylic Acids / Q000737:chemistry; D012997:Solvents; D013056:Spectrophotometry, Ultraviolet; D014046:Tolmetin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D014325:Tromethamine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry
D000180:Acrylic Resins; D000894:Anti-Inflammatory Agents, Non-Steroidal; D002214:Capsules; D011109:Polymethacrylic Acids; D012997:Solvents; D014325:Tromethamine; C038300:methylmethacrylate-methacrylic acid copolymer; D020911:Ketorolac Tromethamine; D014046:Tolmetin